Plasma l-α-acetylmethadol (LAAM) after acute and chronic administration

Gary L. Henderson, B. Kent Wilson, Derick H Lau

Research output: Contribution to journalArticle

40 Scopus citations

Abstract

1-α-Acetvlmethadol (LAAM) was administered orally to two groups of subjects; one group received methadone, 50 rng/day, for three months previously and the other group were heroin addicts who had no prior exposure to methadone or LAAM. Plasma elimination curves for methadone. LAAM, and its metabolites, noracetylmethadol (N-LAAM) and dinoracetylmethadol (DN-LAAM), were determined after acute and chronic administration. The plasma decay curve for LAAM was biexponential (t 1 2α = 6 hr; t 1 2β > 50 hr) following acute or chronic administration. Following chronic administration, N-LAAM abd DN-LAAM plasma levels increased 5- to 10-fold. At this time, N-LAAM had a t 1 2 of 31 hr and DN-LAAM had a t 1 2 of >100 hr. There appear- to be at least two factors which determine the long duration of action of LAAM: metabolic conversion to active metabolites and tissue or plasma binding. Both methadone and LAAM may compete for plasma protein or tissue binding sites. The clinical implications of this potential drug-drug interaction are discussed.

Original languageEnglish (US)
Pages (from-to)16-25
Number of pages10
JournalClinical Pharmacology and Therapeutics
Volume21
Issue number1
StatePublished - Jan 1977

ASJC Scopus subject areas

  • Pharmacology

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